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Sustained release of active molecules from polymers topically applied to skin or hairRelated Patent Categories: Drug, Bio-affecting And Body Treating Compositions, Live Hair Or Scalp Treating Compositions (nontherapeutic), Polymer Containing (nonsurfactant, Natural Or Synthetic)Sustained release of active molecules from polymers topically applied to skin or hair description/claimsThe Patent Description & Claims data below is from USPTO Patent Application 20060088489, Sustained release of active molecules from polymers topically applied to skin or hair. Brief Patent Description - Full Patent Description - Patent Application Claims
[0001] This application claims priority from of U.S. 60/622,583, filed Oct. 27, 2004. FIELD OF THE INVENTION [0002] The invention relates to topical compositions. More specifically, the invention relates to polymeric compositions useful in delivering biologically active materials to the skin and hair. BACKGROUND OF THE INVENTION [0003] Topical application of enzymes, drugs, moisturizers, fragrances, and of other cosmetic or pharmacological molecules has been practiced for centuries in the course of human history. Topical Alpha-chemotrypsin is used to treat hematomas (1), topical salicylic acid at high concentration is used to remove callous bodies (2), whereas at low concentration it helps the natural process of desquamation to yield smooth skin surface (3) and topical vitamin E can be used to reduce the unwanted effects of solar radiation (4). Cosmetics and pharmaceuticals provide countless examples of beneficial effects obtained by topical administration of large variety of ingredients. [0004] Transdermal delivery has recently gained popularity as a route of administration of both cosmetic and pharmaceutical actives, as an alternative to perfusion or systemic. Transdermal delivery has a number of advantages, which include less trauma to the patient in delivery, as well as enabling the use of drugs which, although efficient in treating specific diseases, are toxic for or disabled by the digestive system or which are not appropriate for the perfusion route. This method of delivering active material across the skin does have certain drawbacks and hurdles to overcome in its own right. [0005] One of the major difficulties with transdermal delivery is that, to achieve effective delivery of the active, it often must permeate through the stratum corneum, the epidermis and the basal membranes of the skin. The success in achieving this is dependent upon the lipophilic/hydrophilic character of the material to be delivered (5). One method of circumventing this difficulty is the incorporation and delivery of the active in liposomes, and with liposomes, some success, at least for epidermal delivery, has been achieved (6). [0006] Another major problem in achieving successful transdermal delivery is that a large amount of a drug needed to achieve the therapeutic result must be administered all at once, i.e., all at the moment of application. Depending upon the chemical identity of the active, the effective quantity can cause any number of undesirable effects, such as irritation, inflammation, local toxicity, or apoptosis. This effect is not limited to pharmaceuticals: similarly, suboptimal effects of cosmetic ingredients can also occur when they are applied to the skin or hair in a non-controlled manner. For example, an excess of moisturizer might not provide the desired feeling to dry skin, and an large quantity fragrance might be considered overwhelming or allergy-inducing to some particularly sensitive users. [0007] Thus, there remains a continued need for development of systems for achieving sustained release of topically applied pharmacologic or cosmetic ingredients, with the desired result, among others, of prolonging the duration of the desired effects while avoiding adverse effects and/or expense of the application of large amounts of the free ingredient. The present invention provides a mechanism for achieving that goal. SUMMARY OF THE INVENTION [0008] The present invention relates to a polymer for topical delivery of biologically active ingredients, the polymer comprising at least one moiety: [0009] U-B-A in which U represents a physiologically acceptable unit of an oligomer or a polymer, B represents a bond capable of being disrupted by a biological, physical or chemical process occurring in or on skin, and A represents a biologically active component. As a result of disruption of the bond on the skin, the active ligand is released on the skin in a controlled fashion, rather than all being available simultaneously, and may thus result in a more benign and efficacious delivery of the material than would otherwise be achievable. The invention further provides topical compositions comprising the polymer of the invention, as well as a method of delivering a biologically active material to the skin, comprising applying to the skin a polymer of the invention containing the active material as a component. DESCRIPTION OF THE FIGURES [0010] FIG. 1 is a diagram of the lipase-catalyzed synthesis of oligo .epsilon.-caprolactone) with geraniol esterified at the carboxyl termini of chains. [0011] FIG. 2 is a diagram of the lipase-catalyzed condensation polymerization of sebasic acid, 1,8-octanediol, and anisyl to form poly(1,8-octanylsebacate) with anisyl esters at carboxyl termini of chains. [0012] FIG. 3 is a diagram of the lipase-catalyzed condensation polymerization of adipic acid, sorbitol and anisyl alcohol to form the corresponding polyester with with anisyl esters at carboxyl termini of chains. [0013] FIG. 4 is a diagram of the lipase-catalyzed synthesis of oligo(.epsilon.-caprolactone) with the 2-(4-aminophenyl)ethyl alcohol Schiff base derivative of floralozone at the carboxyl termini of chains [0014] FIG. 5 is a diagram of the synthesis of floralozone glycerol acetal derivative and its conjugation by ester bonds to carboxyl chain ends during lipase-catalyzed synthesis of oligo(.epsilon.-caprolactone). DEFINITIONS [0015] In this specification, various terms are defined as follows: [0016] "Regioselective reactions" are reactions in which at least two constitutional isomers can be formed from single reactant but one isomer is observed to predominate the product of the reaction. Regioselective reactions also can include reactions in which one isomer is formed exclusively. In this invention it refers directly to the selective polymerization of two hydroxyl groups contained within a polyol that has .gtoreq.3 hydroxyl groups. [0017] "Chemical reactions" can include the formation or dissociation of ionic, covalent, or noncovalent structures through known means. Chemical reactions can include changes in environmental conditions such as pH, ionic strength, and temperature. [0018] A "polymer" can be and can include homopolymers, copolymers, and combinations thereof where the average chain length is greater than or equal to 2 repeat units. [0019] An "oligomer" can be and can include homopolymers, copolymers, and combinations thereof where the average chain length is less than or equal to 10 repeat units. [0020] A "polyol" can be any compound in which there are more than two hydroxyl groups. Polyol compounds can include compounds such as carbohydrates. Continue reading about Sustained release of active molecules from polymers topically applied to skin or hair... 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